普罗布考壳聚糖纳米粒子的制备及体外释放  

Preparation of probucol loaded chitosan nanoparticles and in vitro release study

作　　者：高礼[1] 万锕俊[2] 

机构地区：[1]宁夏大学资源环境学院,银川750021 [2]上海交通大学化学化工学院,上海200240

出　　处：《中国新药杂志》2009年第19期1892-1896,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(20376045);上海市纳米专项重点项目(0452nm037)

摘　　要：目的:制备负载普罗布考的壳聚糖纳米粒子,观察其一般特性、载药量、包封率和体外释放特性。方法:将疏水性药物普罗布考溶解于二氯甲烷,滴加到壳聚糖醋酸溶液中,形成O/W微乳液,室温下缓慢滴加三聚磷酸钠(TPP)溶液,交联形成负载普罗布考的壳聚糖纳米粒子。观察其一般特性,计算载药量和包封率,并模拟体内条件研究普罗布考壳聚糖纳米粒子的体外释放特性。结果:纳米粒子表面圆整,粒径在50 nm左右,包封率可达75%以上,载药量在10%左右。药物突释量大小与TPP浓度、壳聚糖浓度以及壳聚糖的相对分子质量有关,释放时间可持续7 d左右。结论:普罗布考壳聚糖纳米粒子制备工艺效果好,具有明显的缓释作用。Objective：To prepare probucol loaded chitosan nanoparticles and investigate their general characteristics,drug release characteristics in vitro. Methods： The nanoparticles were prepared with tripolyphosphate （TPP） by ionic crosslinking. Probucol was dissolved in CH2Cl2 and added in chitosan acetic solutions. An O/W emulsion was formed under drastic stirring. Sodium TPP solution was dropped at room temperature. The probucol loaded chitosan nanoparticles were formed. Their general properties were observed. In vivo conditions were simula- ted to study probucol loaded chitosan nanopartieles release characteristics. Results：The nanoparticles were smooth spherical shape and their diameter was about 50 nm. Encapsulation efficiency of probucol was above 75%. The loading capacity was about 10%. The release behaviors of probucol were affected by various preparation processes, such as concentration of TPP and ehitosan solution. The release experiment of probueol in vitro showed that the nanoparticles provided a sustained release of the entrapped probucol for about 7 days. Conclusion：The prepared probucol loaded chitosan nanoparticals had good properties and offered an optimally sustained release of probucol.

关 键 词：普罗布考 再狭窄 壳聚糖 纳米 

分 类 号：R943.41[医药卫生—药剂学] R972.6[医药卫生—药学]